1233403-74-1Relevant academic research and scientific papers
Discovery of a novel HDAC3 selective inhibitor and its evaluation in lymphoma model
Choi, Chang-Ju,Kim, Mira,Han, Sun Young,Jeon, Jiyoung,Lee, Jae Ho,Oh, Jeong-In,Suh, Kwee Hyun,Suh, Dong-Churl,Lee, Kwang-Ok
, p. 42 - 47 (2016)
Histone deacetylase (HDAC) inhibition is a potentially attractive approach to cancer therapy. A number of HDAC inhibitors are in clinical development stages for the treatment of cancer as well as immune and inflammatory disorders. Although there are several approved HDAC inhibitors by the US FDA, they show a broad inhibitory spectrum against HDAC subfamily. Herein, we synthesized a series of novel hydroxamate analogs, and evaluated them with lymphoma cancer cell. Conclusively, we identified an HDAC3 selective inhibitor which shows good anticancer activity for the lymphoma model, as well as a good drug metabolism and pharmacokinetics (DMPK) profile.
Synthesis of new heteroaryl substituted morpholine tagged triazines and evaluation of their cytotoxic activity
Kasturi, Sivaprasad,Surarapu, Sujatha,Uppalanchi, Srinivas,Anantaraju, Hasitha Shilpa,Dwivedi, Shubham,Yogeeswari, Perumal,Ethiraj, Krishna S.,Anireddy, Jaya Shree
, p. 181 - 192 (2018/03/21)
Background: In the present study, new triazine derivatives 3, 4, 5, 6, 8 and 10 were synthesized starting from readily available cyanuric chloride 1 via nucleophilic displacement with morpholine followed by Suzuki or Stille coupling reactions and then the
NOVEL HYDROXAMATE DERIVATIVES AND PHARMACEUTICAL COMPOSITION FOR TREATMENT OR PREVENTION OF CANCER CONTAINING THE SAME
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Paragraph 0162; 0163, (2017/01/05)
The present invention relates to novel hydroxamate derivatives or pharmaceutically acceptable salts thereof, and a pharmaceutical composition comprising the same as active components for preventing or treating cancers. The novel hydroxamate derivatives or pharmaceutically acceptable salts thereof selectively inhibit histone deacetylase-3 which is involved in delivering signals to control a DNA packing structure in cells, and thus resolve toxicity limit of a conventional pan-HDAc inhibitor while effectively inhibiting growth of cancer cells.COPYRIGHT KIPO 2016
Synyhesis and anti-hepatitis C virus activity of morpholino triazine derivatives
Misawa, Takashi,Salim, Mohammed T.A.,Okamoto, Mika,Baba, Masanori,Aoyama, Hiroshi,Hashimoto, Yuichi,Sugita, Kazuyuki
scheme or table, p. 1419 - 1428 (2010/12/24)
A series of morpholino triazines was synthesized and evaluated for anti-hepatitis C virus (HCV) activity. Incorporation of OMe, CN and F into the phenyl moiety afforded analogues with moderate potency and good selectivity, as assessed with the subgenomic HCV RNA replicon assay.
